Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Nanchang, P.R. China.
University of Chicago, Tang Center for Herbal Medicine Research, and Department of Anesthesia and Critical Care, Chicago, Illinois, USA.
J Appl Biomed. 2021;19(2):113-124. doi: 10.32725/jab.2021.013.
(Nakai) Nakai has a long history of use as an ethnomedicine by the people living in eastern Asia. However, its bioactive constituents and cancer chemopreventive mechanisms are largely unknown. The aim of this study was to prepare extracts, fractions, and single compounds and to investigate the herb's antiproliferative effects on colon cancer cells and the involved mechanisms of action. Two polyyne compounds were isolated from , falcarindiol and oplopandiol. Based on our HPLC analysis, falcarindiol and oplopandiol are major constituents in the dichloromethane (CHCl) fraction. For the HCT-116 cell line, the dichloromethane fraction showed significant effects. Furthermore, the IC50 for falcarindiol and oplopandiol was 1.7 μM and 15.5 μM, respectively. In the mechanistic study, after treatment with 5 μg/ml for 48 h, dichloromethane fraction induced cancer cell apoptosis by 36.5% ( < 0.01% vs. control of 3.9%). Under the same treatment condition, dichloromethane fraction caused cell cycle arrest at the G2/M phase by 32.6% ( < 0.01% vs. control of 23.4%), supported by upregulation of key cell cycle regulator cyclin A to 21.6% ( < 0.01% vs. control of 8.6%). Similar trends were observed by using cell line HT-29. Data from this study filled the gap between phytochemical components and the cancer chemoprevention of . The dichloromethane fraction is a bioactive fraction, and falcarindiol is identified as an active constituent. The mechanisms involved in cancer chemoprevention by were apoptosis induction and G2/M cell cycle arrest mediated by a key cell cycle regulator cyclin A.
(Nakai)Nakai 在东亚地区的民间医学中有着悠久的应用历史。然而，其生物活性成分和抗癌化学预防机制在很大程度上仍是未知的。本研究的目的是制备提取物、馏分和单一化合物，并研究该草药对结肠癌细胞的抗增殖作用及其作用机制。从高丽菜中分离得到两种聚炔类化合物，法卡林二醇和奥洛潘二醇。根据我们的 HPLC 分析，法卡林二醇和奥洛潘二醇是二氯甲烷（CHCl ）馏分的主要成分。对于 HCT-116 细胞系，二氯甲烷馏分表现出显著的效果。此外，法卡林二醇和奥洛潘二醇的 IC50 值分别为 1.7 μM 和 15.5 μM。在机制研究中，用 5μg/ml 的二氯甲烷馏分处理 48 h 后，诱导癌细胞凋亡 36.5%（<0.01%，与对照组的 3.9%相比）。在相同的处理条件下，二氯甲烷馏分使细胞周期停滞在 G2/M 期 32.6%（<0.01%，与对照组的 23.4%相比），这一作用是通过上调细胞周期调控因子细胞周期蛋白 A 到 21.6%（<0.01%，与对照组的 8.6%相比）来支持的。在 HT-29 细胞系中也观察到了类似的趋势。本研究的数据填补了高丽菜的植物化学成分与癌症化学预防之间的空白。二氯甲烷馏分是一种具有生物活性的馏分，法卡林二醇被鉴定为一种活性成分。高丽菜通过诱导细胞凋亡和 G2/M 细胞周期停滞来发挥抗癌作用的机制涉及到关键的细胞周期调控因子细胞周期蛋白 A。
